Antiproliferation activity and the mechanism of action of 9-bromo-5-morpholino-tetrazolo[1,5-c]quinazoline--potential anticancer drug.
9-Bromo-5-morpholino-tetrazolo[1,5-c]quinazoline (BMTQ) at the two highest tested concentrations (74.6; 29.8 mumol@l) induced retarded cytotoxic effect. After 24 hours of culturing 23.1-98.8% of the cell population proliferated but after 48 and 72 hours 6.4-80.4% of the cell population degenerated. Other concentrations induced toxicity that was concentration-and time-dependent. The cytolytic concentrations of BMTQ induced integrity damage of cytoplasmatic membrane. The inhibition of cell cycle and the elevated content of proteins in the cell exposed to the cytotoxic concentrations of BMTQ suggest that the cells synthesize protein without entering into mitosis and that dying cells are in the S-phase before death. BMTQ induced 1.75-3.01 times increase of the level of ssDNA in comparison with the control.
Jantová
S
S
Department of Biochemistry and Microbiology, Faculty of Chemical Technology, Slovak University of Technology, Bratislava, Slovakia.
Ruzeková
L
L
Stankovský
S
S
Spirková
K
K
D000970:Antineoplastic Agents / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D003593:Cytoplasm / Q000648:ultrastructure; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D007425:Intracellular Membranes / Q000187:drug effects; D011799:Quinazolines / Q000494:pharmacology*; D013777:Tetrazoles / Q000494:pharmacology*
C110549:9-bromo-5-morpholino-tetrazole(1,5-c)quinazoline; D000970:Antineoplastic Agents; D011799:Quinazolines; D013777:Tetrazoles